Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

Erik Årstad, Stefan Platzer, Achim Berthele, Lyn S. Pilowsky, Sajinder K. Luthra, Hans Jürgen Wester, Gjermund Henriksen

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

Abstract

Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.

Original languageEnglish
Pages (from-to)6307-6313
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number18
DOIs
StatePublished - 15 Sep 2006
Externally publishedYes

Keywords

  • Amidine
  • Carbon-11
  • Glutamate
  • NMDA-NR2B
  • PET

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